Skp2-Cks1 inhibitor E35

Chemical Structure : Skp2-Cks1 inhibitor E35

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货号: PC-25478Not For Human Use, Lab Use Only.

Skp2-Cks1 inhibitor E35 is a potent small molecule inhibitor of S-phase kinase-associated protein 2 (Skp2), inhbits Skp2-Cks1 protein-protein interaction (PPI) with IC50 of 4.86 uM.

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生物&药学活性

Skp2-Cks1 inhibitor E35 is a potent small molecule inhibitor of S-phase kinase-associated protein 2 (Skp2), inhbits Skp2-Cks1 protein-protein interaction (PPI) with IC50 of 4.86 uM.
E35 directly engages Skp2 in living cells.
E35 directly breaks Skp2-Cks1 in pull-down assays and thermally stabilizes endogenous Skp2 in MGC-803 and PC-3 cells.
E35 significantly inhibits colony formation and migration, as well as arrested the cell cycle at the S-phase.
E35 markedly decreases the expression of Skp2, as well as increased the expression of its substrates p21 and p27.
E35 (25 and 50 mg/kg/2 day, intragastric administration for 21 days) showed an obvious inhibitory effect on MGC-803 xenograft mice without obvious toxicity.

物理化学性质&存储条件

分子量	457.35
分子式	C20H17BrN4O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-((4-bromobenzyl)thio)-7-(2,4-dimethoxyphenyl)-[1,2,4]triazolo[1,5-a]pyrimidine

参考文献

1. Kamel EM, et al. Eur J Pharmacol. 2025 Sep 6:178129.

2. Hu K, et al. J Med Chem. 2024 Sep 26;67(18):16435-16454.